| 主权项 |
1. Compounds of the formula I in which X
denotes H, CH3 or NH2, R1 denotes Ar or Het, R2 denotes pyrazolyl, pyrrolidinyl or cyclopentyl, each of which is unsubstituted or monosubstituted by A, Hal, [C(R3)2]pOR3, O[C(R3)2]pOR3, [C(R3)2]pN(R3)2, [C(R3)2]pAr, [C(R3)2]pHet1, CN, [C(R3)2]pCOOR3, Cyc, CO[C(R3)2]pN(R3)2, CO[C(R3)2]pHet1, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet1, O[C(R3)2]mN(R3)2, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]p-Het1, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet1 or C(O)R3, R3 denotes H or unbranched or branched alkyl with 1-4 C-atoms, Ar
denotes phenyl, which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]pOR3, O[C(R3)2]pOR3, [C(R3)2]pN(R3)2, O[C(R3)2]pN(R3)2, [C(R3)2]pHet1, NO2, CN, [C(R3)2]pCOOR3, O[C(R3)2]pCOOR3, CONH2, CONA, CONA2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet1, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]pHet1, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet1, S(O)nHet1, CHO and/or COA, Het
denotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, indolinyl, benzimidazolyl, indazolyl, quinolyl, isoquinolyl, benzoxazolyl, 1,3-benzodioxolyl, benzothiophenyl, benzofuranyl, imidazopyridyl, dihydroindolyl, quinoxalinyl, benzo[1,2,5]thiadiazolyl or furo[3,2-b]pyridyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, [C(R3)2]pOR3, O[C(R3)2]pOR3, [C(R3)2]pN(R3)2, O[C(R3)2]pN(R3)2, [C(R3)2]pHet1, NO2, CN, [C(R3)2]pCOOR3, O[C(R3)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet1, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]p-Het1, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet1, S(O)nHet1, CHO, COA, ═S and/or ═O, Het1 denotes pyrazolyl, pyridyl, pyrazinyl, indolyl, dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl or piperazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, [C(R3)2]pOR3, O[C(R3)2]pOR3, [C(R3)2]pN(R3)2, [C(R3)2]pHet2, NO2, CN, [C(R3)2]pCOOR3, O[C(R3)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet2, O[C(R3)2]mN(R3)2, O[C(R3)2]pHet2, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]pHet2, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]pHet2, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet2, S(O)nHet2, CHO, COA, ═S and/or ═O, Het2 denotes pyrrolidinyl, azetidinyl, azoxetanyl, tetrahydroimidazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, piperidinyl, morpholinyl, tetrahydropyranyl or piperazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, OA, CN, COOA, CON H2, S(O)nA, S(O)nAr, COA and/or ═O, Cyc
denotes cycloalkyl with 3-7 C-atoms, which is unsubstituted or monosubstituted by NH2, A
denotes unbranched or branched alkyl with 1-6 C-atoms, wherein one or two non-adjacent CH- and/or CH2-groups may be replaced by N-, O- and/or S-atoms and wherein 1-7H-atoms may be replaced by F or Cl, Hal
denotes F, Cl, Br or I, n
denotes 0, 1 or 2, m
denotes 1, 2 or 3,p denotes 0, 1, 2, 3 or 4,and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. |
